overview | Polaris can be used as an intermediate in pharmaceutical synthesis. If you inhale Boris, please move the patient to fresh air; if you are in contact with the skin, you should remove the contaminated clothes, rinse the skin thoroughly with soapy water and water, and see a doctor if you feel uncomfortable; if you are in contact with the eyes, you should separate the eyelids, Rinse with flowing water or normal saline, and see a doctor immediately; if you eat, rinse your mouth immediately, prohibit vomiting, and see a doctor immediately. |
Biological activity | Ponalrestat (ICI 128436) is an orally active, selective and non-competitive aldose reductase (aldose reductase;AKR1B1;ALR) inhibitor. Ponalrestat can selectively inhibit ALR2,Ki is 7.7 nM, and the Ki value for ALR1 is 60 μM. Ponalrestat inhibits the conversion of glucose to sorbitol. |
target | Ki: 7.7 nM (ALR2) and 60 μM (ALR1) |
in vitro study | Ponalrestat (ICI 128436; 1, 10,100 μM; 6 hours) reduces PGF2αproduction in response to IL-1 in both cultured endometrial cells and endometrial explants. |
in vivo study | Ponalrestat (ICI 128436; 10, 50 mg/kg; orally; daily; 8 weeks) reduces sorbitol accumulation indicating efficacy of aldose reductase inhibition. Animal Model: Adult female Sprague-Dawley rats Dosage: 10, 50 mg/kg Administration: Orally; daily; 8 weeks Result: reduced sorbitol accumulation. |
Animal Model:
| Adult female Sprague-Dawley rats |
Dosage:
| 10, 50 mg/kg |
Administration:
| Orally; daily; 8 weeks |
Result:
| Reduced sorbitol accumulation. |